RAF inhibitor PLX8394 selectively disrupts BRAF-dimers and RAS-independent BRAF mutant-driven signaling

Activating BRAF mutants and fusions signal as RAS-independent constitutively active dimers with the exception of BRAF V600 mutant alleles which can function as active monomers(1). Current RAF inhibitors are monomer selective, they potently inhibit BRAF V600 monomers but their inhibition of RAF dimer...

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Veröffentlicht in:Nat Med
Hauptverfasser: Yao, Zhan, Gao, Yijun, Su, Wenjing, Yaeger, Rona, Tao, Jessica, Na, Na, Zhang, Ying, Zhang, Chao, Rymar, Andrey, Tao, Anthony, Timaul, Neilawattie M., Mcgriskin, Rory, Outmezguine, Nathaniel A., Zhao, HuiYong, Chang, Qing, Qeriqi, Besnik, Barbacid, Mariano, de Stanchina, Elisa, Hyman, David M, Bollag, Gideon, Rosen, Neal
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2018
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6404779/
https://ncbi.nlm.nih.gov/pubmed/30559419
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/s41591-018-0274-5
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